"Non-small cell lung cancer is a highly heterogeneous disease
and one of the most difficult cancers to treat. Common genetic
alterations responsible for the disease, such as those driven by
KRAS or certain EGFR mutations, typically render anticancer
treatments powerless,” stated Murray O. Robinson, Ph.D.,
senior vice president, oncology at AVEO. “Utilizing our
proprietary cancer biology platform, we have created and treated
genetically-engineered lung cancer mouse models driven by treatment
resistant EGFR or KRAS, resulting in a much more realistic,
human-like environment in which we can evaluate tivozanib efficacy.
We are very pleased with and encouraged by the robust activity
demonstrated by tivozanib in these difficult-to-treat tumor
alleles."

Tivozanib is a novel, oral triple VEGF receptor inhibitor which
recently completed a Phase 2 clinical study and is expected to
enter a Phase 3 clinical trial later this year in patients with
advanced kidney cancer. Tivozanib is being studied in several
ongoing Phase 1b/2a clinical trials. Clinical results to date
suggest tivozanib is a potent, well tolerated anticancer agent with
broad potential as a treatment for solid tumors.

"Our innovative, proprietary cancer biology platform helps us
create more relevant models of cancer in which we can evaluate the
efficacy of our drug candidates preclinically, thereby increasing
the probability of success in the clinic,” stated Tuan
Ha-Ngoc, president and chief executive officer of AVEO
Pharmaceuticals. “The robust anti-angiogenic and anti-tumor
activity of tivozanib in AVEO-engineered models of TKI-resistant
lung tumors, paired with the early results observed with tivozanib
in patients with lung cancer from the previously reported Phase 1
trial, highlights the potential role of tivozanib in the treatment
of this difficult-to-treat cancer.”

In this study, AVEO developed genetically engineered lung
adenocarcinoma models driven by either treatment resistant
EGFRT790M or KRAS mutant proteins by creating chimeric mice
incorporating genetically modified ES cells. Tumors driven by EGFR
or KRAS were propagated in vivo, to examine tivozanib
activity in both subcutaneous and orthotopic settings. Treatment of
subcutaneous lung KRAS tumors with tivozanib 2mg/kg and 5mg/kg
daily PO for two weeks resulted in complete tumor growth inhibition
and 44 percent tumor regressions respectively. Lung EGFR tumors
were tested in an orthotopic setting by intravenous seeding.
Tivozanib treatment was initiated after tumor establishment was
detected by in vivo imaging; 5 mg/kg daily dosing for more
than 10 days resulted in prolonged survival. Histologic analysis
showed the same dramatic anti-angiogenic changes as in the
subcutaneous KRAS tumors, indicating that tivozanib is effective in
killing orthotopic lung tumors that are resistant to EGFR targeted
kinase inhibitors (TKIs).

In a previously reported Phase 1 dose-escalation study
evaluating tivozanib in 41 patients with advanced solid tumors
clinical benefit (i.e., partial response or stable disease lasting
for three months or longer) was achieved across multiple tumor
types, including in those patients with lung cancer. Overall, tumor
shrinkage was observed in 33 percent of all patients during
treatment with tivozanib. A Phase 1b/2a trial evaluating tivozanib
as monotherapy in patients with non-small cell lung cancer was
initiated in March 2009 and is ongoing.

In May 2009, researchers presented complete Phase 2 data
evaluating tivozanib in metastatic renal cell carcinoma (mRCC) at
the 45th Annual Meeting of the American Society for
Clinical Oncology (ASCO), which demonstrated prolonged
progression-free survival of 11.8 months and an excellent safety
profile in patients treated with tivozanib. The company expects to
initiate a Phase 3 trial of tivozanib in advanced kidney cancer
later this year.

About Tivozanib

Tivozanib (AV-951), an investigational new drug, is a novel,
highly potent and selective inhibitor of VEGF receptors 1, 2 and 3,
exhibiting picomolar inhibitory activity against all three
receptors. Angiogenesis inhibition has demonstrated benefit for
patients with a wide range of cancer types, including renal cell
carcinoma, metastatic breast cancer, colorectal cancer, and
non-small cell lung cancer. Due to its potency and
specificity, AVEO believes tivozanib may enable maximal inhibition
of the VEGF pathway, while avoiding side effects associated with
off-target activity. Such a profile may enable tivozanib to be more
readily combined with standard chemotherapy as well as other
targeted therapies, potentially increasing the breadth of its
clinical utility. In addition, AVEO has evaluated tivozanib
using its Human Response Platform (HRP™), a unique set of
engineered tumor models that provide further insight into potential
clinical settings, combinability with other anti-cancer agents,
tumor subtypes and responsive patient populations.

AVEO recently completed a Phase 2 placebo-controlled, randomized
discontinuation trial assessing the efficacy and safety of
once-daily, oral tivozanib in renal cell carcinoma (RCC). In
addition, AVEO is currently conducting multiple ongoing clinical
trials of tivozanib including a Phase 1b trial in combination with
temsirolimus (Torisel™), an approved mTOR inhibitor, in
patients with mRCC; a Phase 1b trial in combination with the
FOLFOX6 chemotherapy regimen in patients with advanced colorectal
cancer and other gastrointestinal cancers; a Phase 1b/2a trial in
combination with paclitaxel (Taxol™) in patients with
metastatic breast cancer; and a Phase 1b/2a trial as monotherapy in
patients with non-small cell lung cancer.

About AVEO

AVEO is a late-stage biopharmaceutical company focused on the
discovery and development of novel, targeted cancer therapeutics.
AVEO's proprietary, integrated cancer biology platform enables the
company to pursue highly efficient drug development strategies in
oncology that increase the probability of clinical success and
provides a discovery engine for high-value targets and therapies.
This approach has resulted in a balanced pipeline of novel cancer
therapies focused on well-validated targets (VEGFR, EGFR) and
promising novel targets (HGF, FGFR, ErbB3 and NOTCH), as well as
collaborations with Eli Lilly, Merck, OSI Pharmaceuticals,
Schering-Plough and Biogen Idec. The company's lead product,
tivozanib (AV-951), a triple VEGF receptor inhibitor, recently
completed Phase 2 clinical development in patients with metastatic
renal cell cancer and is expected to enter Phase 3 development in
2009. Through a combination of internal drug discovery and
selective in-licensing of targeted therapeutics, AVEO is building a
diversified product pipeline and moving toward its vision of
becoming a fully integrated biopharmaceutical company. For more
information, please visit the company's website at
www.aveopharma.com.

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